Synthesis of a tritium-labeled photo-affinity probe based on an atypical leukotriene biosynthesis inhibitor
✍ Scribed by Nag S. Kumar; Matthew P. Braun; Ashok G. Chaudhary; Robert N. Young
- Publisher
- John Wiley and Sons
- Year
- 2011
- Tongue
- French
- Weight
- 207 KB
- Volume
- 54
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
A radiolabeled photo‐affinity probe containing a diazirine group was designed and synthesized based on an atypical leukotriene (LT) biosynthesis inhibitor to determine whether this type of inhibitor (such as 5) interacts with a novel protein, critical for LT biosynthesis. One of the key transformations was to introduce a tritium label in the thiazole ring. This was eventually achieved by treating the iodinated compound with tritium, Pt/C (sulfided) and triethylamine in anhydrous aprotic solvent, to give the tritiated compound with a specific activity of 303 GBq/mmol. The affinity probe will be used to identify the proteins and protein complexes with which this type of molecules interacts with in inflammatory cells. Copyright © 2010 John Wiley & Sons, Ltd.